Velcicky, Juraj, Feifel, Roland, Hawtin, Stuart, Heng, Richard, Huppertz, Christine, Koch, Guido, Kroemer, Markus, Moebitz, Henrik, Revesz, Laszlo, Scheufler, Clemens and Schlapbach, Achim (2009) Novel 3-Aminopyrazole Inhibitors of MK-2 Discovered by Scaffold Hopping Strategy. Bioorganic and Medicinal Chemistry Letters, 20 (3). pp. 1293-1297. ISSN 0960-894X

Abstract

New, selective 3-aminopyrazole based MK2-inhibitors were discovered by scaffold hopping strategy. The new derivatives proved to inhibit intracellular phosphorylation of hsp27 as well as LPS-induced TNFa release in cells. In addition, selected derivative 14e also inhibited LPS-induced TNFa release in vivo.

Item Type:	Article
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez...
Additional Information:	Author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords:	MK2; TNFα-inhibition; 3-Aminopyrazole; Scaffold hopping; Induced-fit; X-ray
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez...
Date Deposited:	13 Oct 2015 13:17
Last Modified:	13 Oct 2015 13:17
URI:	https://oak.novartis.com/id/eprint/1178